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WO/2000/035860A2 |
The subject invention involves novel acyl isothiocyanate resins of formula (I) and processes for making them: (a) starting with a phenyl carboxy resin, treating the resin with any reagent that converts the carboxy to an acyl halide, foll...
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WO/2000/035861A1 |
Bis-amido polybiguanides and their use as antimicrobial agents in pharmaceutical compositions are disclosed. A method of synthesis of bis-amido polybiguanides is also disclosed. The bis-amido polybiguanides are useful in the preservation...
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WO/2000/035868A2 |
Methods for the synthesis of $g(a)-hydroxy-$g(b)-amino acid and amide derivatives and $g(a)-ketoamide derivatives and novel derivatives made by these methods are provided. These methods involve reacting an N-terminally blocked (protected...
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WO/2000/035862A1 |
Amido polybiguanides and their use as antimicrobial agents in pharmaceutical compositions are disclosed. A method of synthesis of amido polybiguanides is also disclosed. The amido polybiguanides are useful in the preservation of pharmace...
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WO2000012454A9 |
A cationic lipid for transfection of macromolecules in which the lipid has a polyether or glyceryl backbone which lipids can be contained in a liposome to effectively transfect a variety of cell types and improve the efficiency of transf...
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WO/2000/032560A1 |
A composition for use in protecting or improving a skin which comprises a polymer having a structure represented by formula (9), wherein each of R1, R2 and R3 independently represents a hydrogen atom, or an alkyl, an alkyloxy or an alkyl...
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WO/2000/030624A2 |
(57) Abstract The invention relates to the use of benzoylguanidines of formula (I) wherein R?1¿ is A; R?2¿ is Het, C¿n?F¿m?H¿2n+1-m?O¿p?, R?4¿, OR?4¿, OH, benzyl, CN, Hal, SO¿q?-R?5¿, Ph, O-Ph, O-Het, NH-Het, NH¿2?, NHA, NA¿2...
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WO/2000/030444A1 |
The present invention relates to synthetic cationic lipids, liposome formulations and the use of such compounds to introduce functional bioactive agents into cultured cells.
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WO/2000/031025A1 |
The invention relates to a method of producing N-alkyl-N'-nitroguanidine. According to said method, an alkyl amine solution is added to a nitroguanidine or nitroguanidine nitrate suspension at temperatures of $m(g) 60 °C and the ammonia...
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WO/2000/031046A1 |
The invention concerns compounds of formula (I) wherein: m = 1, 2 or 3; n = 1, 2 or 3; R¿5? represents a group selected among COR¿6?, CO¿2?R¿6?, SO¿2?R¿6?, SO¿2?NHR¿6?, SO¿2?NHCOR¿6?, SO¿2?NHCO¿2?R¿6?, CONH¿2? and CONHR¿6?...
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WO/2000/027795A1 |
Disclosed are compounds capable of facilitating transport of biologically active agents or substances into cells having general structure (A).
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WO/2000/028328A1 |
New cyclopentane and cyclopentene compounds are provided along with their use in method for detecting influenza virus.
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WO/2000/021920A1 |
Compounds of the formula (1a), wherein R1 is a group of the formula (2) where R1, R2, A, B, U, V, W, X, Y, Z, k and n have the significance given in the specification, are useful to treat rheumatoid arthritis, psoriasis, multiple scleros...
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WO/2000/017152A1 |
Amine derivatives represented by general formula (1) and preparations for external use containing the same which exhibit excellent effects of preventing the skin from aging, etc. In formula (1), R?1¿ represents C¿1-30? hydrocarbyl opti...
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WO/2000/014048A1 |
Compounds of the invention having general formula (I) are useful reagents for protecting amine, guanidine, amidine or hydroxyl groups during organic synthesis. In particular, compounds are useful during oligonucleotide synthesis to prote...
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WO/2000/009115A1 |
Novel GRP receptor antagonists are provided. Methods of using the present compounds to antagonize GRP receptors are also provided. The present invention further involves the synthesis of the present compounds.
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WO/2000/009129A1 |
Novel C3A ligands are provided. Methods of using the present compounds to treat immune and inflammation disease are also provided.
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WO/2000/009116A1 |
Novel GRP receptor antagonists are provided. Methods of using the present compounds to antagonize GRP receptors are also provided. The present invention further involves the synthesis of the present compounds.
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WO/2000/003734A1 |
Therapeutic and/or preventive agents for allergic diseases, particularly, allergy type I and IV reactions, inflammation, rhinitis, conjunctivitis, bronchial asthma, atopic diseases (such as dermatitis or enteritis) and allergic inflammat...
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WO/2000/001676A1 |
This invention relates to novel potassium channel blocking agents, and their use in the preparation of pharmaceutical compositions. Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation...
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WO/2000/001383A1 |
RGD mimetics which combine a nitroaryl moiety with an arylether/$g(a)-aminoacid/guanidine framework exhibit activity as antagonists toward various integrins and as inhibitors of angiogenesis.
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WO/1999/067206A1 |
Compounds of general formula (I) are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular...
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WO/1999/067205A1 |
Compounds of general formula (I) are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular...
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WO/1999/067203A1 |
Compounds of general formula (I) wherein A is (a) or (b); Z is (CH¿2?)¿m? or a carbonyl group are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions compris...
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WO/1999/065882A1 |
The invention relates to compounds having formula (I), wherein R?1¿, R?2¿, R?3¿, R?4¿, A?1¿, A?2¿, X and n have the meanings defined in Claim 1. Said compounds and the salts thereof are suitable as herbicides and plant growth regul...
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WO/1999/061414A1 |
Compounds represented by general formula (1) which are useful as remedies and preventives for diseases caused by acceleration in the sodium/proton exchange system, wherein R¿1?, R¿2?, R¿3?, R¿4? and R¿5? represent each hydrogen, alk...
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WO/1999/058497A1 |
Guanidine and diaminonitroethene derivatives represented by formula (I), wherein X, R?1¿, R?2¿, R?3¿ and R?4¿ are defined in the description, compositions thereof and methods for preparing the compounds described. The compounds are u...
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WO/1999/057096A1 |
The invention relates to novel compounds of formula (I), wherein X, R?1¿, R?2¿, R?3¿, R?4¿ and R?5¿ have the meanings cited in Patent Claim No. 1. Said compounds are inhibitors of the coagulation factor Xa and can be used for prophy...
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WO/1999/055690A1 |
This invention relates to guanidine derivatives of formula (I) wherein each symbol is as defined in the description, and its pharmaceutically acceptable salt, to processes for preparation thereof, to pharmaceutical composition comprising...
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WO/1999/055355A1 |
The present invention is directed to aminoguanidine and alkoxyguanidine compounds, including compounds of Formula (I) wherein X is O or NR?19¿ and A?1¿, A?2¿, R?7¿-R?10¿, R?18¿, R?a¿, R?b¿, R?c¿, n and m are set forth in the spe...
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WO/1999/054279A1 |
This invention relates to a series of substituted amino acids of formula (I), pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention are small molecules which bind to the e...
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WO/1999/054291A1 |
The invention relates to a method for producing a disinfectant based on polyhexamethylene guanidine by the interaction of hexamethylene diamine and guanidine hydrochloride during heating. The hexamethylene diamine and guanidine hydrochlo...
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WO/1999/052879A1 |
Compounds of formula (I) are useful in the treatment of various disorders including, but not limited to, cancer, angiogenesis, restenosis, inflammation, bone diseases, and as antiviral agents. Novel methods of makings compounds of formul...
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WO/1999/052861A1 |
The invention relates to novel benzyl guanidine derivatives for therapy and $i(in-vivo) and $i(in-vitro) diagnosis. The invention also relates to the use of these compounds as therapeutic agents and diagnostic agents, especially for trea...
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WO/1999/051571A1 |
The present invention is directed to aminoguanidine and alkoxyguanidine compounds, including compounds of Formula (I), wherein X is O or NH, L is -O- or -SO¿2?-, and R?1¿-R?4¿, R?9¿-R?19¿, R?a¿, R?b¿, R?c¿, Y, Z, n and m are set ...
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WO/1999/051564A1 |
This invention relates to new propanolamine derivatives or salts thereof represented by general formula (I), wherein each symbol is as defined in the specification or salts thereof which are $g(b)¿3? adrergenic receptor agonists and the...
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WO/1999/046316A2 |
The present invention relates to compounds, compositions, and methods which are useful for the prevention and treatment of adverse health, skin, hair, and oral conditions. The compounds, compositions, and methods are also widely applicab...
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WO/1999/044987A1 |
Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are of general formula (I), where X¿1?, X¿2?, Y, and Z are defined variables. Such compounds and their pharmaceutically acceptable salts, multim...
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WO/1999/043312A1 |
A stable aqueous solution of creatine acid sulfate provides a source of creatine to an animal when taken orally. The aqueous solution of creatine acid sulfate (after neutralization and buffering) has a pH of about 7.2 to about 7.8 and is...
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WO/1999/040073A2 |
The invention relates to bifunctional inhibitors of human tryptase of formula (I), to human tryptase in crystalline form, to a method for producing human tryptase in crystalline form, to pharmaceutical compositions comprising a bifunctio...
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WO/1999/040083A2 |
The invention relates to compounds of formula (I), wherein M, A1, A2, A3, A4, A5, A6, B1, B2, B3, B4, B5, B6, K1 and K2 have the meanings given in the description. Said compounds are novel effective inhibitors of human tryptase.
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WO/1999/037294A2 |
The present invention relates generally to mitochondria protecting agents for treating diseases in which mitochondrial dysfunction leads to tissue degeneration and, more specifically, to compounds, compositions and methods related to the...
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WO/1999/033460A1 |
Acyl guanidines are provided which are sodium/proton exchange (NHE) inhibitors which have structure (I) wherein n is 1 to 5; X is N or C-R?5¿ wherein R?5¿ is H, halo, alkenyl, alkynyl, alkoxy, alkyl, aryl or heteroaryl; and R?1¿, R?2Â...
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WO/1999/033781A1 |
Compounds represented by formulae (I, II or III), wherein U is CH, O, or S; Z is -C(R¿2?)(R¿3?), -CH-N(R¿2?)(R¿3?), C(R¿3?)[(CH¿2?)nR¿2?], CH-C(R¿3?)(R¿8?)(CH¿2?)nR¿2?, C[(CH¿2?)nR¿2?]-[CH(R¿3?)(R¿8?)], C[(R¿3?)][CH[(CH¿...
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WO/1999/032158A2 |
Aminobiguanides and the use of same as antimicrobial agents in pharmaceutical compositions are disclosed. The aminobiguanides are useful in the preservation of pharmaceutical compositions, particularly ophthalmic pharmaceutical compositi...
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WO/1999/032457A1 |
The present invention relates to acylguanidine derivatives of formula (I) in which R?1¿, R?2¿, R?4¿, R?5¿, R?6¿, A, m and n have the meanings indicated in the patent claims, their physiologically tolerable salts and their prodrugs. ...
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WO/1999/032433A1 |
The present invention provides compounds of formula (I). The present invention also provides methods of treating or preventing inflammation or atherosclerosis, and a pharmaceutical composition that contains a compound of formula (I).
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WO/1999/031049A1 |
Compounds of formula (I) wherein: Q represents an amidino group, a cyano group or a group of formula XYN-, (where X and Y are hydrogen or various groups); R?a¿ represents alkylene; R?b¿ and R?c¿ each represents alkylene, the total num...
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WO/1999/031052A1 |
Compounds having not only a high metalloproteinase inhibitory activity but also remarkably improved medicinal applicability $i(in vivo) (oral absorbability, etc.) and biological activities and thus being useful as drugs; intermediates in...
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WO/1999/029677A1 |
The invention relates to novel substituted 2,4-diamino-1,3,5-triazines of formula (I) in which Q represents O (oxygen), S (sulfur), SO, SO¿2?, NH or N(alkyl), R?1¿ represents hydrogen or optionally substituted alkyl, R?2¿ represents h...
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